EPI-001

EPI-001 is an androgen receptor antagonist with an IC₅₀ value of approximately 6 μM for inhibition of transactivation of the androgen receptor N-terminal domain (NTD).¹ It inhibits androgen-, FSK-, and IL-6-induced, as well as ligand-independent, prostate-specific antigen (PSA) reporter gene expression in LNCaP cells expressing either the full length androgen receptor or a constitutively active mutant that lacks the ligand binding domain in a dose-dependent manner. EPI-001 inhibits androgen receptor interaction with the PSA androgen response element and blocks androgen-stimulated induction of endogenous PSA and 17 other androgen regulated genes in LNCaP cells. It inhibits androgen-dependent and -independent growth of LNCaP and MDA-PCa-2B cells, but not 22Rv1, DU145, or PC3 cells that do not express the androgen receptor. EPI-001 (50 mg/kg) reduces serum PSA and tumor growth in an LNCaP prostate cancer xenograft model in castrated mice. It also reduces serum PSA in a patient-derived LT313 prostate cancer mouse xenograft model. Formulations containing EPI-001 are under clinical investigation for the treatment of castration-resistant prostate cancer.

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1. Andersen, R.J., Mawji, N.R., Wang, J., et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell 17(6), 535-546 (2010).